| S7070 |
GSK-J4 Hydrochloride
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GSK J4 HCl is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family.
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Mol Cell, 2025, 85(15):2973-2987.e6
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Nat Cell Biol, 2024, 26(7):1165-1175
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J Clin Invest, 2024, 134(24)e173403
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| S7281 |
JIB-04
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JIB-04 (NSC 693627) is a pan-selective Jumonji histone demethylase inhibitor with IC50 of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D in cell-free assays, respectively. This compound also induces cell apoptosis.
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Mol Cell, 2025, 85(15):2973-2987.e6
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J Immunother Cancer, 2025, 13(10)e013269
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Front Cell Dev Biol, 2025, 13:1566567
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| S8287 |
CPI-455 HCl
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CPI-455 HCl is a specific KDM5 inhibitor with a half-maximal inhibitory concentration (IC50) of 10 ± 1 nM for full-length KDM5A in enzymatic assays, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents.
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Nature, 2023, 622(7983):619-626
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Cancer Cell, 2023, 41(6):1118-1133.e12
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EBioMedicine, 2023, 92:104602
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| S7234 |
IOX1
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IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. This compound is an inhibitor of ALKBH5.
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Mol Cell, 2025, 85(15):2973-2987.e6
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Cancer Gene Ther, 2025, 10.1038/s41417-025-00874-z
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Front Immunol, 2024, 15:1308978
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| S7581 |
GSK J1
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GSK-J1 is a highly potent inhibitor of H3K27 histone demethylase JMJD3 (KDM6B) and UTX (KDM6A) with IC50 of 60 nM in cell-free assays for JMJD3 (KDM6B) , respectively, >10-fold selectivity over other tested demethylases, with IC50 of 0.95μM and 1.76μM towards JARID1B/C.
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Cancer Gene Ther, 2025, 10.1038/s41417-025-00874-z
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Commun Biol, 2025, 8(1):269
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Chem Biol Interact, 2025, 418:111576
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| S7296 |
ML324
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ML324 is a selective inhibitor of jumonji histone demethylase (JMJD2) with IC50 of 920 nM.
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Mol Cell, 2025, 85(15):2973-2987.e6
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Cancer Cell, 2023, 41(6):1118-1133.e12
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EBioMedicine, 2023, 92:104602
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| S8601 |
CP2
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CP2 is a cyclic peptide that inhibits the JmjC histone demethylases KDM4 with IC50 values of 42 nM and 29 nM for KDM4A and KDM4C, respectively.
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Clin Mol Hepatol, 2025, 10.3350/cmh.2024.0694
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Oxid Med Cell Longev, 2022, 2022:2405943
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Front Cell Dev Biol, 2021, 9:697614
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| S0201 |
Z-JIB-04 (NSC 693627)
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Z-JIB-04 (NSC 693627, JIB-04 Z-isomer) is an isomer of JIB-04. JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50 of 230 nM, 340 nM, 855 nM, 445 nM, 435 nM, 1100 nM and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively.
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Mol Cell, 2025, 85(15):2973-2987.e6
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Cell Death Discov, 2025, 11(1):326
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| E1315 |
iJMJD6
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iJMJD6(WL12) is an inhibitor of arginine demethylase JMJD6 with an IC50 value of 0.22 μM.
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| S4800New |
Daminozide
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Daminozide (Aminozide, DMASA, DIMG, B 995, Alar, Kylar, B-NINE, SADH) is a plant growth regulator that selectively inhibits human KDM2/7 histone demethylases, with IC50 of 0.55 μM for PHF8 (KDM7B), 1.5 μM for KDM2A, and 2.1 μM for KIAA1718 (KDM7A). It shows over 100-fold selectivity for the KDM2/7 subfamily compared to other histone demethylase subfamilies, with significantly weaker activity against enzymes such as KDM3A with IC50 of 127 μM.
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